COMPOUNDS AND COMPOSITIONS INTENDED FOR THE TREATMENT OF PATHOLOGICAL CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

Description

TECHNICAL FIELD

[0001] This disclosure features chemical entities (e.g., a compound that modulates (e.g., antagonizes) NLRP3, or a pharmaceutically acceptable salt, and / or hydrate, and / or cocrystal, and / or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in NLRP3 activity (e.g., an increase, e.g., a condition, disease or disorder associated with NLRP3 signaling) contributes to the pathology and / or symptoms and / or progression of the condition, disease or disorder in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

[0002] References to methods of treatment in the summary and detailed description of the invention in this description are to be interpreted as references to the compounds, pharmaceutical compositions and medicaments of the present invention for use in a method for treatment of the human (or animal) body by therapy (or for diagnosis).BACKGROUND

[0003] The NLRP3 inflammasome is a component of the inflammatory process and its aberrant activation is pathogenic in inherited disorders such as the cryopyrin associated periodic syndromes (CAPS). The inherited CAPS Muckle-Wells syndrome (MWS), familial cold autoinflammatory syndrome (FCAS) and neonatal onset multi-system inflammatory disease (NOMID) are examples of indications that have been reported to be associated with gain of function mutations in NLRP3.

[0004] NLRP3 can form a complex and has been implicated in the pathogenesis of a number of complex diseases, including but not limited to metabolic disorders such as type 2 diabetes, atherosclerosis, obesity and gout, as well as diseases of the central nervous system, such as Alzheimer's disease and multiple sclerosis and Amyotrophic Lateral Sclerosis and Parkinson disease, lung disease, such as asthma and COPD and pulmonary idiopathic fibrosis, liver disease, such as NASH syndrome, viral hepatitis and cirrhosis, pancreatic disease, such as acute and chronic pancreatitis, kidney disease, such as acute and chronic kidney injury, intestinal disease such as Crohn's disease and Ulcerative Colitis, skin disease such as psoriasis, musculoskeletal disease such as scleroderma, vessel disorders, such as giant cell arteritis, disorders of the bones, such as Osteoarthritis , osteoporosis and osteopetrosis disorders eye disease, such as glaucoma and macular degeneration, diseased caused by viral infection such as HIV and AIDS, autoimmune disease such as Rheumatoid Arthritis, Systemic Lupus Erythematosus, Autoimmune Thyroiditis, Addison's disease, pernicious anemia, cancer and aging.

[0005] WO2016 / 131098 describes sulfonylurea compounds as NLRP3 inhibitors. EP 2 927 214 A1 describes nitrogen-containing heterocyclic compounds useful for the treatment of skin diseases. J. Med. Chem., Toth J.E. et al., vol. 40, no. 6, 14 March 1997, pages 1018-1025, describes sulfonimidamide analogs of oncolytic sulfonylureas. J. Org. Chem., 1993, 58, 3469-3472, describes the synthesis and resolution of sulfonimidamide analogs of sulfonylureas. EP0552553A1 describes sulfonimidamides as antineoplastic agents. Bioorg. & Med. Chem. Letters 10 (2000), pages 1887-1891, describes arylsulfonyl-N,N-diethyl-dithiocarbamates as antitumor agents. Eur. J. of Med. Chem., vol. 35, issue 9, September 2000, pages 867-874, describes carbonic anhydrase inhibitors - 1,3,4-thiadiazole-2-sulfonamide derivatives as anitumor agents. Oxidation Communications, vol. 26, no. 1, 2003, pages 9-13, discusses antitumor activity of sulfonamidamide analogs of oncolytic sulfonylureas. EP 2 314 593 A1 describes platelet ADP receptor inhibitors. EP 0 173 498 A1 describes herbicidal sulfonimidamide compounds. WO2017 / 184604 A1, WO2017 / 184623 A1 and WO 2017 / 184624 A1 describe compounds as NLRP3 inhibitors. WO2018 / 225018 A1 describes substituted suloximine compounds. WO2019 / 068772 A1 describes sulfonimidamide compounds for treating conditions associated with NLRP activity.

[0006] In light of the above, it would be desirable to provide compounds that modulate (e.g., antagonize) NLRP3.SUMMARY

[0007] This disclosure features chemical entities (e.g., a compound that modulates (e.g., antagonizes) NLRP3, or a pharmaceutically acceptable salt, and / or hydrate, and / or cocrystal, and / or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in NLRP3 activity (e.g., an increase, e.g., a condition, disease or disorder associated with NLRP3 signaling).

[0008] In some embodiments, provided herein is a compound of Formula AA or a pharmaceutically acceptable salt thereof, wherein the variables in Formula AA can be as defined anywhere herein.

[0009] This disclosure also features compositions as well as other methods of using and making the same.

[0010] An "antagonist" of NLRP3 includes compounds that inhibit the ability of NLRP3 to induce the production of IL-1β and / or IL-18 by directly binding to NLRP3, or by inactivating, destabilizing, altering distribution, of NLRP3 or otherwise.

[0011] In one aspect, pharmaceutical compositions are featured that include a chemical entity described herein (e.g., a compound described generically or specifically herein or a pharmaceutically acceptable salt thereof or compositions containing the same) and one or more pharmaceutically acceptable excipients.

[0012] Embodiments can include one or more of the following features.

[0013] The chemical entity can be administered in combination with one or more additional therapies with one or more agents suitable for the treatment of the condition, disease or disorder.

[0014] Examples of the indications that may be treated by the compounds disclosed herein include but are not limited to metabolic disorders such as type 2 diabetes, atherosclerosis, obesity and gout, as well as diseases of the central nervous system, such as Alzheimer's disease and multiple sclerosis and Amyotrophic Lateral Sclerosis and Parkinson disease, lung disease, such as asthma and COPD and pulmonary idiopathic fibrosis, liver disease, such as NASH syndrome, viral hepatitis and cirrhosis, pancreatic disease, such as acute and chronic pancreatitis, kidney disease, such as acute and chronic kidney injury, intestinal disease such as Crohn's disease and Ulcerative Colitis, skin disease such as psoriasis, musculoskeletal disease such as scleroderma, vessel disorders, such as giant cell arteritis, disorders of the bones, such as osteoarthritis , osteoporosis and osteopetrosis disorders, eye disease, such as glaucoma and macular degeneration, diseases caused by viral infection such as HIV and AIDS, autoimmune disease such as rheumatoid arthritis, systemic Lupus erythematosus, autoimmune thyroiditis; Addison's disease, pernicious anemia, cancer and aging.

[0015] Other embodiments include those described in the Detailed Description and / or in the claims.Additional Definitions

[0016] To facilitate understanding of the disclosure set forth herein, a number of additional terms are defined below. Generally, the nomenclature used herein and the laboratory procedures in organic chemistry, medicinal chemistry, and pharmacology described herein are those well-known and commonly employed in the art. Unless defined otherwise, all technical and scientific terms used herein generally have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs.

[0017] As used herein, the term "NLRP3" is meant to include, without limitation, nucleic acids, polynucleotides, oligonucleotides, sense and antisense polynucleotide strands, complementary sequences, peptides, polypeptides, proteins, homologous and / or orthologous NLRP3 molecules, isoforms, precursors, mutants, variants, derivatives, splice variants, alleles, different species, and active fragments thereof.

[0018] The term "acceptable" with respect to a formulation, composition or ingredient, as used herein, means having no persistent detrimental effect on the general health of the subject being treated.

[0019] "API" refers to an active pharmaceutical ingredient.

[0020] The terms "effective amount" or "therapeutically effective amount," as used herein, refer to a sufficient amount of a chemical entity (e.g., a compound exhibiting activity as a modulator of NLRP3, or a pharmaceutically acceptable salt and / or hydrate and / or cocrystal thereof;) being administered which will relieve to some extent one or more of the symptoms of the disease or condition being treated. The result includes reduction and / or alleviation of the signs, symptoms, or causes of a disease, or any other desired alteration of a biological system. For example, an "effective amount" for therapeutic uses is the amount of the composition comprising a compound as disclosed herein required to provide a clinically significant decrease in disease symptoms. An appropriate "effective" amount in any individual case is determined using any suitable technique, such as a dose escalation study.

[0021] The term "excipient" or "pharmaceutically acceptable excipient" means a pharmaceutically-acceptable material, composition, or vehicle, such as a liquid or solid filler, diluent, carrier, solvent, or encapsulating material. In one embodiment, each component is " pharmaceutically acceptable" in the sense of being compatible with the other ingredients of a pharmaceutical formulation, and suitable for use in contact with the tissue or organ of humans and animals without excessive toxicity, irritation, allergic response, immunogenicity, or other problems or complications, commensurate with a reasonable benefit / risk ratio. See, e.g., Remington: The Science and Practice of Pharmacy, 21st ed.; Lippincott Williams & Wilkins: Philadelphia, PA, 2005; Handbook of Pharmaceutical Excipients, 6th ed.; Rowe et al., Eds.; The Pharmaceutical Press and the American Pharmaceutical Association: 2009; Handbook of Pharmaceutical Additives, 3rd ed.; Ash and Ash Eds.; Gower Publishing Company: 2007; Pharmaceutical Preformulation and Formulation, 2nd ed.; Gibson Ed.; CRC Press LLC: Boca Raton, FL, 2009.

[0022] The term "pharmaceutically acceptable salt" may refer to pharmaceutically acceptable addition salts prepared from pharmaceutically acceptable non-toxic acids including inorganic and organic acids. In certain instances, pharmaceutically acceptable salts are obtained by reacting a compound described herein, with acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, ethanesulfonic acid, p-toluenesulfonic acid, salicylic acid and the like. The term "pharmaceutically acceptable salt" may also refer to pharmaceutically acceptable addition salts prepared by reacting a compound having an acidic group with a base to form a salt such as an ammonium salt, an alkali metal salt, such as a sodium or a potassium salt, an alkaline earth metal salt, such as a calcium or a magnesium salt, a salt of organic bases such as dicyclohexylamine, N-methyl-D-glucamine, tris(hydroxymethyl)methylamine, and salts with amino acids such as arginine, lysine, and the like, or by other methods previously determined. The pharmacologically acceptable salt s not specifically limited as far as it can be used in medicaments. Examples of a salt that the compounds described hereinform with a base include the following: salts thereof with inorganic bases such as sodium, potassium, magnesium, calcium, and aluminum; salts thereof with organic bases such as methylamine, ethylamine and ethanolamine; salts thereof with basic amino acids such as lysine and ornithine; and ammonium salt. The salts may be acid addition salts, which are specifically exemplified by acid addition salts with the following: mineral acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, and phosphoric acid:organic acids such as formic acid, acetic acid, propionic acid, oxalic acid, malonic acid, succinic acid, fumaric acid, maleic acid, lactic acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, and ethanesulfonic acid; acidic amino acids such as aspartic acid and glutamic acid.

[0023] The term "pharmaceutical composition" refers to a mixture of a compound described herein with other chemical components (referred to collectively herein as "excipients"), such as carriers, stabilizers, diluents, dispersing agents, suspending agents, and / or thickening agents. The pharmaceutical composition facilitates administration of the compound to an organism. Multiple techniques of administering a compound exist in the art including, but not limited to: rectal, oral, intravenous, aerosol, parenteral, ophthalmic, pulmonary, and topical administration.

[0024] The term "subject" refers to an animal, including, but not limited to, a primate (e.g., human), monkey, cow, pig, sheep, goat, horse, dog, cat, rabbit, rat, or mouse. The terms "subject" and "patient" are used interchangeably herein in reference, for example, to a mammalian subject, such as a human.

[0025] The terms "treat," "treating," and "treatment," in the context of treating a disease or disorder, are meant to include alleviating or abrogating a disorder, disease, or condition, or one or more of the symptoms associated with the disorder, disease, or condition; or to slowing the progression, spread or worsening of a disease, disorder or condition or of one or more symptoms thereof.

[0026] The terms "hydrogen" and "H" are used interchangeably herein.

[0027] The term "halo" refers to fluoro (F), chloro (Cl), bromo (Br), or iodo (I).

[0028] The term "alkyl" refers to a hydrocarbon chain that may be a straight chain or branched chain containing the indicated number of carbon atoms. For example, C 1-10 indicates that the group may have from 1 to 10 (inclusive) carbon atoms in it. Non-limiting examples include methyl, ethyl, iso-propyl, tert-butyl, n-hexyl.

[0029] The term "haloalkyl" refers to an alkyl, in which one or more hydrogen atoms is / are replaced with an independently selected halo.

[0030] The term "alkoxy" refers to an -O-alkyl radical (e.g., -OCH 3 ).

[0031] The term "carbocyclic ring" as used herein includes an aromatic or nonaromatic cyclic hydrocarbon group having 3 to 10 carbons, such as 3 to 8 carbons, such as 3 to 7 carbons, which may be optionally substituted. Examples of carbocyclic rings include five-membered, six-membered, and seven-membered carbocyclic rings.

[0032] The term "heterocyclic ring" refers to an aromatic or nonaromatic 5-8 membered monocyclic, 8-12 membered bicyclic, or 11-14 membered tricyclic ring system having 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S (e.g., carbon atoms and 1-3, 1-6, or 1-9 heteroatoms of N, O, or S if monocyclic, bicyclic, or tricyclic, respectively), wherein 0, 1, 2, or 3 atoms of each ring may be substituted by a substituent. Examples of heterocyclic rings include five-membered, six-membered, and seven-membered heterocyclic rings.

[0033] The term "cycloalkyl" as used herein includes an nonaromatic cyclic, bicylic, fused, or spiro hydrocarbon radical having 3 to 10 carbons, such as 3 to 8 carbons, such as 3 to 7 carbons. Examples of cycloalkyls include five-membered, six-membered, and seven-membered rings. Examples include cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, and cyclooctyl.

[0034] The term "heterocycloalkyl" refers to an nonaromatic 5-8 membered monocyclic, 8-12 membered bicyclic, or 11-14 membered tricyclic ring, fused, or spiro system radical having 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S (e.g., carbon atoms and 1-3, 1-6, or 1-9 heteroatoms of N, O, or S if monocyclic, bicyclic, or tricyclic, respectively). Examples of heterocycloalkyls include five-membered, six-membered, and seven-membered heterocyclic rings. Examples include piperazinyl, pyrrolidinyl, dioxanyl, morpholinyl, tetrahydrofuranyl, and the like.

[0035] The term "aryl" is intended to mean an aromatic ring radical containing 6 to 10 ring carbons. Examples include phenyl and naphthyl.

[0036] The term "heteroaryl" is intended to mean an aromatic ring system containing 5 to 14 aromatic ring atoms that may be a single ring, two fused rings or three fused rings wherein at least one aromatic ring atom is a heteroatom selected from, but not limited to, the group consisting of O, S and N. Examples include furanyl, thienyl, pyrrolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, pyrazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, triazinyl and the like. Examples also include carbazolyl, quinolizinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, triazinyl, indolyl, isoindolyl, indazolyl, indolizinyl, purinyl, naphthyridinyl, pteridinyl, carbazolyl, acridinyl. phenazinyl, phenothiazinyl, phenoxazinyl, benzoxazolyl, benzothiazolyl, 1H-benzimidazolyl, imidazopyridinyl, benzothienyl, benzofuranyl, isobenzofuran and the like.

[0037] The term "hydroxy" refers to an OH group.

[0038] The term "amino" refers to an NH 2 group.

[0039] The term "oxo" refers to O. By way of example, substitution of a CH 2 a group with oxo gives a C=O group.

[0040] As used herein, the terms "the ring A" or "A" are used interchangeably to denote in formula AA, wherein the bond that is shown as being broken by the wavy line connects A to the S(O)(NHR 3< )=N moiety of Formula AA.

[0041] As used herein, the terms "the ring B" or "B" are used interchangeably to denote in formula AA wherein the bond that is shown as being broken by the wavy line connects B to the NH(CO) group of Formula AA.

[0042] As used herein, the term "the optionally substituted ring A" is used to denote in formula AA, wherein the bond that is shown as being broken by the wavy line connects A to the S(O)(NHR 3< )=N moiety of Formula AA.

[0043] As used herein, the term "the substituted ring B" is used to denote in formula AA, wherein the bond that is shown as being broken by the wavy line connects B to the NH(CO) group of Formula AA.

[0044] As used herein, the recitation "S(O 2 )", alone or as part of a larger recitation, refers to the group

[0045] In addition, atoms making up the compounds of the present embodiments are intended to include all isotopic forms of such atoms. Isotopes, as used herein, include those atoms having the same atomic number but different mass numbers. By way of general example and without limitation, isotopes of hydrogen include tritium and deuterium, and isotopes of carbon include 13< C and 14< C.

[0046] The scope of the compounds disclosed herein includes tautomeric form of the compounds. Thus, by way of example, a compound that is represented as containing the moiety is also intended to include the tautomeric form containing the moiety In addition, by way of example, a compound that is represented as containing the moiety is also intended to include the tautomeric form containing the moiety

[0047] Non-limiting exemplified compounds of the formulae described herein include a stereogenic sulfur atom and optionally one or more stereogenic carbon atoms. This disclosure provides examples of stereoisomer mixtures (e.g., racemic mixture of enantiomers; mixture of diastereomers). This disclosure also describes and exemplifies methods for separating individual components of said stereoisomer mixtures (e.g., resolving the enantiomers of a racemic mixture). In cases of compounds containing only a stereogenic sulfur atom, resolved enantiomers are graphically depicted using one of the two following formats: formulas A / B (hashed and solid wedge three-dimensional representation); and formula C ("flat structures with *-labelled stereogenic sulfur).

[0048] In reaction schemes showing resolution of a racemic mixture, Formulas A / B and C are intended only to convey that the constituent enantiomers were resolved in enantiopure pure form (about 98% ee or greater). The schemes that show resolution products using the formula A / B format are not intended to disclose or imply any correlation between absolute configuration and order of elution. Some of the compounds shown in the tables below are graphically represented using the formula A / B format. However, with the exception of compounds 181a and 181b , the depicted stereochemistry shown for each of the tabulated compounds drawn in the formula A / B format is a tentative assignment and based, by analogy, on the absolute stereochemistry assigned to compounds 181b (see, e.g., FIGS. 1 and 2).

[0049] The details of one or more embodiments of the invention are set forth in the accompanying drawings and the description below. Other features and advantages of the invention will be apparent from the description and drawings, and from the claims.DESCRIPTION OF DRAWINGS

[0050] FIG. 1 depicts ball-and-stick representations of two crystallographically independent molecules of compound 181a in the asymmetrical unit. FIG. 2 depicts ball-and-stick representations of two crystallographically independent molecules of compound 181b in the asymmetrical unit. FIG. 3 depicts the layout of the microplate used in an hTHP-1 assay. DETAILED DESCRIPTION

[0051] In some embodiments, provided herein is a compound of Formula AA wherein m = 0, 1, or 2; n=0, 1, or 2; o = 2; p = 0, 1, 2, or 3; wherein A is a 5-10-membered heteroaryl or a C 6 -C 10 aryl; B is any one of wherein R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC 2 -C 6 alkynyl, NHCOOCC 1 -C 6 alkyl, NH-(C=NR 13< )NR 11< R 12< , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O)C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< wherein the C 1 -C 6 alkyl and C 1 -C 6 alkoxy are optionally substituted with hydroxy, halo, oxo, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl and 3- to 10-membered heterocycloalkyl, and a C 2 -C 6 alkenyl, wherein R 6< and R 7< are each optionally substituted with one or more substituents independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC 2 -C 6 alkynyl, C 6 -C 10 aryloxy, and S(O 2 )C 1 -C 6 alkyl; and wherein the C 1 -C 6 alkyl or C 1 -C 6 alkoxy that R 6< or R 7< is substituted with is optionally substituted with one or more hydroxyl, C 6 -C 10 aryl or NR 8< R 9< , or wherein R 6< or R 7< is optionally fused to a five- to -seven-membered carbocyclic ring or heterocyclic ring containing one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; each of R 4< and R 5< is independently selected from hydrogen and C 1 -C 6 alkyl; R 10< is C 1 -C 6 alkyl; each of R 8< and R 9< at each occurrence is independently selected from hydrogen, C 1 -C 6 alkyl, (C-NR 13< )NR 11< R 12< , S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , COR 13< , CO 2 R 13< and CONR 11< R 12< ; wherein the C 1 -C 6 alkyl is optionally substituted with one or more hydroxy, halo, C 1 -C 6 alkoxy, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, C 3 -C 7 cycloalkyl or 3- to 7-membered heterocycloalkyl; or R 8< and R 9< taken together with the nitrogen they are attached to form a 3- to 7-membered ring optionally containing one or more heteroatoms in addition to the nitrogen they are attached to; R 13< is C 1 -C 6 alkyl, C 6 -C 10 aryl, or 5- to 10-membered heteroaryl; each of R 11< and R 12< at each occurrence is independently selected from hydrogen and C 1 -C 6 alkyl; R 3< is selected from hydrogen; and R 14< is hydrogen, C 1 -C 6 alkyl, 5- to 10-membered monocyclic or bicyclic heteroaryl or C 6 -C 10 monocyclic or bicyclic aryl, wherein each C 1 -C 6 alkyl, aryl or heteroaryl is optionally independently substituted with 1 or 2 R 6< , and wherein the term "alkyl" refers to a hydrocarbon chain that may be a straight chain or branched chain, saturated or unsaturated, containing the indicated number of carbon atoms; or a pharmaceutically acceptable salt thereof.

[0052] In some embodiments the variables shown in the formulae herein are as follows:The variables m and n

[0053] In some embodiments m=0, 1, or 2.

[0054] In some embodiments m=0 or 1.

[0055] In some embodiments m=1 or 2.

[0056] In some embodiments m=0 or 2.

[0057] In some embodiments m=0.

[0058] In some embodiments m=1.

[0059] In some embodiments m=2.

[0060] In some embodiments n=0, 1, or 2.

[0061] In some embodiments n=0 or 1.

[0062] In some embodiments n=1 or 2.

[0063] In some embodiments n=0 or 2.

[0064] In some embodiments n=0.

[0065] In some embodiments n=1.

[0066] In some embodiments n=2.

[0067] In some embodiments, m=0 and n=0.

[0068] In some embodiments, m=1 and n=0.

[0069] In some embodiments, m=1 and n=1.The Ring A and substitutions on the ring A

[0070] In some embodiments, A is a 5- to 6-membered monocyclic heteroaryl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< ; wherein A is any one of: furanyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< ; thiophenyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< ; oxazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< ; thiazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< ; phenyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0071] In some embodiments, A is a 5- to 10-membered (e.g., 5- to 6-membered) monocyclic or bicyclic heteroaryl or a C 6 -C 10 (e.g., C 6 ) monocyclic or bicyclic aryl, such as phenyl.

[0072] In some embodiments, A is a 5- to 10-membered (e.g., 5- to 6-membered) monocyclic or bicyclic heteroaryl.

[0073] In some embodiments, A is a 5-membered heteroaryl containing a sulfur and optionally one or more nitrogens.

[0074] In some embodiments, A is a C 6 -C 10 monocyclic or bicyclic aryl.

[0075] In some embodiments, A is phenyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0076] In some embodiments, A is naphthyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0077] In some embodiments, A is furanyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 R 2< .

[0078] In some embodiments, A is furanyl optionally substituted with 1 R 1< and optionally substituted with 1 or 2 R 2< .

[0079] In some embodiments, A is thiophenyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0080] In some embodiments, A is oxazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0081] In some embodiments, A is thiazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0082] In some embodiments, A is oxazolyl optionally substituted with 2 R 1< or optionally substituted with 2 R 2< .

[0083] In some embodiments, A is thiazolyl optionally substituted with 2 R 1< or optionally substituted with 2 R 2< .

[0084] In some embodiments, A is pyrazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0085] In some embodiments, A is pyrazolyl optionally substituted with 1 R 1< and optionally substituted with 1 or 2 R 2< .

[0086] In some embodiments, A is pyrazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 R 2< .

[0087] In some embodiments, A is pyridyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0088] In some embodiments, A is indazolyl optionally substituted with 1 or 2 R 1< and optionally substituted with 1 or 2 R 2< .

[0089] In some embodiments, A is phenyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0090] In some embodiments, A is naphthyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0091] In some embodiments, A is furanyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0092] In some embodiments, A is thiophenyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0093] In some embodiments, A is oxazolyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0094] In some embodiments, A is thiazolyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0095] In some embodiments, A is pyrazolyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0096] In some embodiments, A is pyridyl substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0097] In some embodiments, A is indazolyl optionally substituted with 1 R 1< and optionally substituted with 1 R 2< .

[0098] In some embodiments, A is phenyl substituted with 1 R 1< and substituted with 1 R 2< .

[0099] In some embodiments, A is furanyl substituted with 1 R 1< and substituted with 1 R 2< .

[0100] In some embodiments, A is thiophenyl substituted with 1 R 1< and substituted with 1 R 2< .

[0101] In some embodiments, A is oxazolyl substituted with 1 R 1< and substituted with 1 R 2< .

[0102] In some embodiments, A is thiazolyl substituted with 1 R 1< and substituted with 1 R 2< .

[0103] In some embodiments, A is pyrazolyl substituted with 1 R 1< and substituted with 1 R 2< .

[0104] In some embodiments, A is pyridyl substituted with 1 R 1< and substituted with 1 R 2< .

[0105] In some embodiments, A is phenyl, m is 0 or 1, and n is 0, 1, or 2.

[0106] In some embodiments, A is furanyl, m is 0 or 1, and n is 0, 1, or 2.

[0107] In some embodiments, A is thiophenyl, m is 0 or 1, and n is 0, 1, or 2.

[0108] In some embodiments, A is oxazolyl, m is 0 or 1, and n is 0, 1, or 2.

[0109] In some embodiments, A is thiazolyl, m is 0 or 1, and n is 0, 1, or 2.

[0110] In some embodiments, A is pyrazolyl, m is 0 or 1, and n is 0, 1, or 2.

[0111] In some embodiments, A is pyridyl, m is 0 or 1, and n is 0, 1, or 2.

[0112] In some embodiments, A is indazolyl, m is 0 or 1, and n is 0, 1, or 2.

[0113] In some embodiments, A is phenyl, m is 0, and n is 0 or 1.

[0114] In some embodiments, A is furanyl, m is 0, and n is 0 or 1.

[0115] In some embodiments, A is thiophenyl, m is 0, and n is 0 or 1.

[0116] In some embodiments, A is oxazolyl, m is 0, and n is 0 or 1.

[0117] In some embodiments, A is thiazolyl, m is 0, and n is 0 or 1.

[0118] In some embodiments, A is pyrazolyl, m is 0, and n is 0 or 1.

[0119] In some embodiments, A is pyridyl, m is 0, and n is 0 or 1.

[0120] In some embodiments, A is one of the rings disclosed hereinbelow optionally substituted as disclosed hereinbelow, wherein in each case the bond that is shown as being broken by the wavy line connects A to the S(O)(NR 3< R 3< )=N moiety of Formula AA.

[0121] In some embodiments, m is 1 and n is 0; wherein A is any one of: or

[0122] In some embodiments, wherein m is 1 and n is 1; wherein A is any one of:

[0123] In some embodiments, wherein m is 2 and n is 1; wherein A is any one of:

[0124] In some embodiments, the optionally substituted ring A is

[0125] In some embodiments, the optionally substituted ring A is

[0126] In some embodiments, the optionally substituted ring A is

[0127] In some embodiments, the optionally substituted ring A is

[0128] In some embodiments, the optionally substituted ring A is

[0129] In some embodiments, the optionally substituted ring A is

[0130] In some embodiments, the optionally substituted ring A is

[0131] In some embodiments, the optionally substituted ring A is

[0132] In some embodiments, the optionally substituted ring A is

[0133] In some embodiments, the optionally substituted ring A is

[0134] In some embodiments, the optionally substituted ring A is

[0135] In some embodiments, the optionally substituted ring A is

[0136] In some embodiments, the optionally substituted ring A is

[0137] In some embodiments, the optionally substituted ring A is

[0138] In some embodiments, the optionally substituted ring A is

[0139] In some embodiments, the optionally substituted ring A is

[0140] In some embodiments, the optionally substituted ring A is

[0141] In some embodiments, the optionally substituted ring A is

[0142] In some embodiments, the optionally substituted ring A is

[0143] In some embodiments, the optionally substituted ring A is

[0144] In some embodiments, the optionally substituted ring A is

[0145] In some embodiments, the optionally substituted ring A is

[0146] In some embodiments, the optionally substituted ring A is

[0147] In some embodiments, the optionally substituted ring A is

[0148] In some embodiments, the optionally substituted ring A is

[0149] In some embodiments, the optionally substituted ring A is

[0150] In some embodiments, the optionally substituted ring A is

[0151] In some embodiments, the optionally substituted ring A is

[0152] In some embodiments, the optionally substituted ring A is

[0153] In some embodiments, the optionally substituted ring A is

[0154] In some embodiments, the optionally substituted ring A is

[0155] In some embodiments, the optionally substituted ring A is

[0156] In some embodiments, the optionally substituted ring A is

[0157] In some embodiments, the optionally substituted ring A is

[0158] In some embodiments, the optionally substituted ring A is

[0159] In some embodiments, the optionally substituted ring A is

[0160] In some embodiments, the optionally substituted ring A is

[0161] In some embodiments, the optionally substituted ring A is

[0162] In some embodiments, the optionally substituted ring A is

[0163] In some embodiments, the optionally substituted ring A is

[0164] In some embodiments, the optionally substituted ring A is

[0165] In some embodiments, the optionally substituted ring A is

[0166] In some embodiments, the optionally substituted ring A is

[0167] In some embodiments, the optionally substituted ring A is

[0168] In some embodiments, the optionally substituted ring A is

[0169] In some embodiments, the optionally substituted ring A is

[0170] In some embodiments, the optionally substituted ring A is

[0171] In some embodiments, the optionally substituted ring A is

[0172] In some embodiments, the optionally substituted ring A is

[0173] In some embodiments, the optionally substituted ring A is

[0174] In some embodiments, the optionally substituted ring A is

[0175] In some embodiments, the optionally substituted ring A is

[0176] In some embodiments, the optionally substituted ring A is

[0177] In some embodiments, the optionally substituted ring A is

[0178] In some embodiments, the optionally substituted ring A is

[0179] In some embodiments, the optionally substituted ring A is

[0180] In some embodiments, the optionally substituted ring A is

[0181] In some embodiments, the optionally substituted ring A is

[0182] In some embodiments, the optionally substituted ring A is

[0183] In some embodiments, the optionally substituted ring A is

[0184] In some embodiments, the optionally substituted ring A is

[0185] In some embodiments, the optionally substituted ring A is

[0186] In some embodiments, the optionally substituted ring A is

[0187] In some embodiments, the optionally substituted ring A is

[0188] In some embodiments, the optionally substituted ring A is

[0189] In some embodiments, the optionally substituted ring A is

[0190] In some embodiments, the optionally substituted ring A is

[0191] In some embodiments, the optionally substituted ring A is

[0192] In some embodiments, the optionally substituted ring A is

[0193] In some embodiments, the optionally substituted ring A is

[0194] In some embodiments, the optionally substituted ring A is

[0195] In some embodiments, the optionally substituted ring A is

[0196] In some embodiments, the optionally substituted ring A is

[0197] In some embodiments, the optionally substituted ring A is

[0198] In some embodiments, the optionally substituted ring A is

[0199] In some embodiments, the optionally substituted ring A is

[0200] In some embodiments, the optionally substituted ring A is

[0201] In some embodiments, the optionally substituted ring A is

[0202] In some embodiments, the optionally substituted ring A is

[0203] In some embodiments, the optionally substituted ring A is

[0204] In some embodiments, the optionally substituted ring A is The groups R 1< and R 2<

[0205] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), and OCO(3- to 7-membered heterocycloalkyl); wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, and 5- to 10-membered heteroaryl are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to-8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ;

[0206] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ;

[0207] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0208] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0209] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each C 1 -C 6 alkyl substituent and each C 1 -C 6 alkoxy substituent of the R 1< or R 2< C 3 -C 7 cycloalkyl or of the R 1< or R 2< 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, or oxo; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to-8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0210] In some embodiments, R 1< and R 2< are independently selected from the group consisting of C 1 -C 6 alkyl optionally substituted with one or more hydroxy, halo, oxo, C 1 -C 6 alkoxy, or NR 8< R 9< ; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, halo, oxo, C 1 -C 6 alkoxy, C 1 -C 6 alkyl, or NR 8< R 9< wherein the C 1 -C 6 alkoxy or C 1 -C 6 alkyl is further optionally substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, halo, oxo, C 1 -C 6 alkyl, or NR 8< R 9< wherein the C 1 -C 6 alkoxy or C 1 -C 6 alkyl is further optionally substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; CO-C 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl; and S(O 2 )C 1 -C 6 alkyl.

[0211] In some embodiments, R 1< is selected from the group consisting of 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; S(O 2 )CH 3 ; and S(O 2 )NR 11< R 12< .

[0212] In some embodiments, R 2< is selected from the group consisting of fluoro, chloro, cyano, methyl; methoxy; ethoxy; isopropyl; 1-hydroxy-2-methylpropan-2-yl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; COCH 3 ; COPh; 2-methoxy-2-propyl; (dimethylamino)methyl; S(O 2 )CH 3 ; and S(O 2 )NR 11< R 12< .

[0213] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl.

[0214] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl are each unsubstituted; or at least one pair of R 1< and R 2< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to-8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ;

[0215] In some embodiments, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, S(O)C 1 -C 6 alkyl, 5- to 10-membered heteroaryl, and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy and oxo.

[0216] In some embodiments, m=1; n=0; and R 1< is selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl.

[0217] In some embodiments , m=1; n=0; and, R 1< is selected from C 1 -C 6 alkyl, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, S(O)C 1 -C 6 alkyl, and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy and oxo.

[0218] In some embodiments, m=1; n=1; and R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO-C 6 -C 10 aryl, CO(5- to 10-membered heteroaryl), CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , S(O)C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl;

[0219] In some embodiments , m=1; n=1; and, R 1< and R 2< are each independently selected from C 1 -C 6 alkyl, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, S(O)C 1 -C 6 alkyl, and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy and oxo.

[0220] In some embodiments, m=1; n=1; and R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 4 -C 8 carbocyclic ring or a 5- to-8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0221] In some embodiments, m=1; n=1; and R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 carbocyclic ring or a 5-to-6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0222] In some embodiments, m=1; n=1; and R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 5 carbocyclic ring or a 5- to-6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0223] In some embodiments, m=1; n=1; and R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is unsubstituted.Particular embodiments wherein m=1 and n=0:

[0224] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy.

[0225] In some embodiments, R 1< is 1-hydroxy-2-methylpropan-2-yl.

[0226] In some embodiments, R 1< is 2-hydroxyethyl.

[0227] In some embodiments, R 1< is C 1 -C 6 alkyl.

[0228] In some embodiments, R 1< is methyl.

[0229] In some embodiments, R 1< is isopropyl.

[0230] In some embodiments, R 1< is isopropyl.

[0231] In some embodiments, R 1< is C 1 -C 6 alkyl substituted with hydroxy at the carbon directly connected to ring A.

[0232] In some embodiments, R 1< is 2-hydroxy-2-propyl.

[0233] In some embodiments, R 1< is hydroxymethyl.

[0234] In some embodiments, R 1< is 1-hydroxyethyl.

[0235] In some embodiments, R 1< is 1-hydroxy-2-propyl.

[0236] In some embodiments, R 1< is C 1 -C 6 alkyl substituted with two or more hydroxy groups.

[0237] In some embodiments, R 1< is C 1 -C 6 alkyl substituted with two or more hydroxy groups, wherein one of the two or more hydroxy groups is bonded to the carbon directly connected to ring A.

[0238] In some embodiments, R 1< is 1,2-dihydroxy-prop-2-yl.

[0239] In some embodiments, R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy.

[0240] In some embodiments, R 1< is C 3 -C 7 cycloalkyl.

[0241] In some embodiments, R 1< is C 3 -C 7 cycloalkyl substituted with hydroxy at the carbon directly connected to ring A.

[0242] In some embodiments, R 1< is 1-hydroxy-1-cyclopropyl.

[0243] In some embodiments, R 1< is 1-hydroxy-1-cyclobutyl.

[0244] In some embodiments, R 1< is 1-hydroxy-1-cyclopentyl.

[0245] In some embodiments, R 1< is 1-hydroxy-1-cyclohexyl.

[0246] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy.

[0247] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl.

[0248] In some embodiments, R 1< is morpholinyl (e.g., 1-morpholinyl).

[0249] In some embodiments, R 1< is 1,3-dioxolan-2-yl.

[0250] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more C 1 -C 6 alkyl.

[0251] In some embodiments, R 1< is 1-methylpyrrolidin-2-yl.

[0252] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl substituted with hydroxy at the carbon directly connected to ring A.

[0253] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo.

[0254] In some embodiments, R 1< is COCH 3 .

[0255] In some embodiments, R 1< is COCH 2 CH 3 .

[0256] In some embodiments, R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more oxo.

[0257] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more oxo.

[0258] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy.

[0259] In some embodiments, R 1< is 2-methoxy-2-propyl.

[0260] In some embodiments, R 1< is methoxymethyl.

[0261] In some embodiments, R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more C 1 -C 6 alkoxy.

[0262] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more C 1 -C 6 alkoxy.

[0263] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< .

[0264] In some embodiments, R 1< is C 1 -C 6 alkyl substituted with NR 8< R 9< at the carbon directly connected to ring A.

[0265] In some embodiments, R 1< is (methylamino)methyl.

[0266] In some embodiments, R 1< is (dimethylamino)methyl.

[0267] In some embodiments, R 1< is aminomethyl.

[0268] In some embodiments, R 1< is N-methylacetamidomethyl.

[0269] In some embodiments, R 1< is 1-(dimethylamino)eth-1-yl.

[0270] In some embodiments, R 1< is 2-(dimethylamino)prop-2-yl.

[0271] In some embodiments, R 1< is (2-methoxy-eth-1-yl)(methyl)aminomethyl.

[0272] In some embodiments, R 1< is (methyl)(acetyl)aminomethyl.

[0273] In some embodiments, R 1< is (methyl)(cyclopropylmethyl)aminomethyl.

[0274] In some embodiments, R 1< is (methyl)(2,2-difluoroeth-1-yl)aminomethyl.

[0275] In some embodiments, R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more NR 8< R 9< .

[0276] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more NR 8< R 9< .

[0277] In some embodiments, R 1< is C 1 -C 6 haloalkyl optionally substituted with one or more hydroxy.

[0278] In some embodiments, R 1< is C 1 -C 6 alkoxy.

[0279] In some embodiments, R 1< is C 1 -C 6 haloalkoxy.

[0280] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with 3- to 7-membered heterocycloalkyl, wherein the 3- to 7-membered heterocycloalkyl is further optionally substituted as defined elsewhere herein.

[0281] In some embodiments, R 1< is pyrrolidinylmethyl (e.g., pyrrolidin-1-ylmethyl).

[0282] In some embodiments, R 1< is optionally substituted pyrrolidinylmethyl (e.g., 3,3-difluoropyrrolidin-1 -ylmethyl).

[0283] In some embodiments, R 1< is azetidinylmethyl (e.g., azetidin-1-ylmethyl).

[0284] In some embodiments, R 1< is optionally substituted azetidinylmethyl (e.g., 3-methoxyazetidin-1-ylmethyl).

[0285] In some embodiments, R 1< is morpholinylmethyl (e.g., morpholin-4-ylmethyl).

[0286] In some embodiments, R 1< is halo.

[0287] In some embodiments, R 1< is fluoro.

[0288] In some embodiments, R 1< is chloro.

[0289] In some embodiments, R 1< is CN.

[0290] In some embodiments, R 1< is NO 2 .

[0291] In some embodiments, R 1< is COC 1 -C 6 alkyl.

[0292] In some embodiments, R 1< is CO-C 6 -C 10 aryl.

[0293] In some embodiments, R 1< is CO(5- to 10-membered heteroaryl).

[0294] In some embodiments, R 1< is CO 2 C 1 -C 6 alkyl.

[0295] In some embodiments, R 1< is CO 2 C 3 -C 8 cycloalkyl.

[0296] In some embodiments, R 1< is OCOC 1 -C 6 alkyl.

[0297] In some embodiments, R 1< is OCOC 6 -C 10 aryl.

[0298] In some embodiments, R 1< is OCO(5- to 10-membered heteroaryl).

[0299] In some embodiments, R 1< is OCO(3- to 7-membered heterocycloalkyl).

[0300] In some embodiments, R 1< is C 6 -C 10 aryl.

[0301] In some embodiments, R 1< is phenyl.

[0302] In some embodiments, R 1< is 5- to 10-membered heteroaryl.

[0303] In some embodiments, R 1< is pyridyl (e.g., 4-pyridyl).

[0304] In some embodiments, R 1< is pyrazolyl (e.g., 1-pyrazolyl).

[0305] In some embodiments, R 1< is NH 2 .

[0306] In some embodiments, R 1< is NHC 1 -C 6 alkyl.

[0307] In some embodiments, R 1< is N(C 1 -C 6 alkyl) 2 .

[0308] In some embodiments, R 1< is CONR 8< R 9< .

[0309] In some embodiments, R 1< is SF 5 .

[0310] In some embodiments, R 1< is SC 1 -C 6 alkyl,

[0311] In some embodiments, R 1< is S(O 2 )C 1 -C 6 alkyl.

[0312] In some embodiments, R 1< is S(O 2 )CH 3 .

[0313] In some embodiments, R 1< is S(O 2 )NR 11< R 12< .

[0314] In some embodiments, R 1< is S(O 2 )N(CH 3 ) 2 .

[0315] In some embodiments, R 1< is S(O)C 1 -C 6 alkyl.

[0316] In some embodiments, R 1< is S(O)CH 3 .

[0317] In some embodiments, R 1< is attached to a carbon of an aryl ring A.

[0318] In some embodiments, R 1< is attached to a carbon of a heteroaryl ring A.

[0319] In some embodiments, R 1< is attached to a nitrogen of a heteroaryl ring A.Particular embodiments wherein m=1 and n=1:

[0320] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy.

[0321] In some embodiments, R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl.

[0322] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is methyl.

[0323] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl.

[0324] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl.

[0325] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl.

[0326] In some embodiments, R 1< is hydroxymethyl and R 2< is methyl.

[0327] In some embodiments, R 1< is 1-hydroxyethyl and R 2< is methyl.

[0328] In some embodiments, R 1< is 2-hydroxyethyl and R 2< is methyl.

[0329] In some embodiments, R 1< is 1-hydroxy-2-propyl and R 2< is methyl.

[0330] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl.

[0331] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is phenyl.

[0332] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl.

[0333] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl.

[0334] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl.

[0335] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 .

[0336] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SC 1 -C 6 alkyl,

[0337] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl.

[0338] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )CH 3 .

[0339] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo.

[0340] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is chloro.

[0341] In some embodiments, R 1< is 2-hydroxy-2-propyl and R 2< is fluoro.

[0342] In some embodiments, R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl.

[0343] In some embodiments, R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl.

[0344] In some embodiments, R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl.

[0345] In some embodiments, R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl.

[0346] In some embodiments, R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl.

[0347] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl.

[0348] In some embodiments, R 1< is morpholinyl, and R 2< is methyl.

[0349] In some embodiments, R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl.

[0350] In some embodiments, R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo.

[0351] In some embodiments, R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro.

[0352] In some embodiments, R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro.

[0353] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl.

[0354] In some embodiments, R 1< is COCH 3 , and R 2< is methyl.

[0355] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl.

[0356] In some embodiments, R 1< is 2-methoxy-2-propyl, and R 2< is methyl.

[0357] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl.

[0358] In some embodiments, R 1< is (dimethylamino)methyl, and R 2< is methyl.

[0359] In some embodiments, R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo.

[0360] In some embodiments, R 1< is (dimethylamino)methyl, and R 2< is fluoro.

[0361] In some embodiments, R 1< is (dimethylamino)methyl, and R 2< is fluoro.

[0362] In some embodiments, R 1< is (methylamino)methyl, and R 2< is fluoro.

[0363] In some embodiments, R 1< is aminomethyl, and R 2< is fluoro.

[0364] In some embodiments, R 1< is C 1 -C 6 alkyl, and R 2< is C 1 -C 6 alkyl.

[0365] In some embodiments, R 1< is methyl, and R 2< is methyl.

[0366] In some embodiments, R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl.

[0367] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is methyl.

[0368] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl.

[0369] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl.

[0370] In some embodiments, R 2< is hydroxymethyl and R 1< is methyl.

[0371] In some embodiments, R 2< is 1-hydroxyethyl and R 1< is methyl.

[0372] In some embodiments, R 2< is 2-hydroxyethyl and R 1< is methyl.

[0373] In some embodiments, R 2< is 1-hydroxy-2-propyl and R 1< is methyl.

[0374] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl.

[0375] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is phenyl.

[0376] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl.

[0377] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl.

[0378] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl.

[0379] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 .

[0380] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SC 1 -C 6 alkyl.

[0381] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl.

[0382] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 .

[0383] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo.

[0384] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is chloro.

[0385] In some embodiments, R 2< is 2-hydroxy-2-propyl and R 1< is fluoro.

[0386] In some embodiments, R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl.

[0387] In some embodiments, R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl.

[0388] In some embodiments, R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl.

[0389] In some embodiments, R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl.

[0390] In some embodiments, R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl.

[0391] In some embodiments, R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl.

[0392] In some embodiments, R 2< is morpholinyl, and R 1< is methyl.

[0393] In some embodiments, R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl.

[0394] In some embodiments, R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo.

[0395] In some embodiments, R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro.

[0396] In some embodiments, R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro.

[0397] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl.

[0398] In some embodiments, R 2< is COCH 3 , and R 1< is methyl.

[0399] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0400] In some embodiments, R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0401] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl.

[0402] In some embodiments, R 2< is (dimethylamino)methyl, and R 1< is methyl.

[0403] In some embodiments, R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo.

[0404] In some embodiments, R 2< is (dimethylamino)methyl, and R 1< is fluoro.

[0405] In some embodiments, R 2< is (methylamino)methyl, and R 1< is fluoro.

[0406] In some embodiments, R 2< is aminomethyl, and R 1< is fluoro.

[0407] In some embodiments, R 2< is C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< .

[0408] In some embodiments, R 2< is methoxy, and R 1< is (dimethylamino)methyl.

[0409] In some embodiments, R 1< and R 2< are each attached to a carbon of an aryl ring A.

[0410] In some embodiments, R 1< and R 2< are each attached to a carbon of a heteroaryl ring A.

[0411] In some embodiments, R 1< is attached to a carbon and R 2< is attached to a nitrogen of a heteroaryl ring A.

[0412] In some embodiments, R 2< is attached to a carbon and R 1< is attached to a nitrogen of a heteroaryl ring A.

[0413] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 5 carbocyclic ring optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0414] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 5 aliphatic carbocyclic ring.

[0415] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 carbocyclic ring optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0416] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 aliphatic carbocyclic ring.

[0417] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 aromatic carbocyclic ring.

[0418] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0419] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0420] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0421] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0422] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0423] In some embodiments, R 1< and R 2< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0424] In some embodiments, R 1< and R 2< are different.

[0425] In some embodiments, R 1< and R 2< are different, and R 2< comprises a carbonyl group.

[0426] In some embodiments, R 1< and R 2< are different, and R 2< comprises 1 or 2 (e.g., 1) nitrogen atoms.

[0427] In some embodiments, R 1< and R 2< are different, and R 2< comprises 1 or 2 (e.g., 1) oxygen atoms.

[0428] In some embodiments, R 1< and R 2< are different, and R 2< comprises a sulfur atom.

[0429] In some embodiments, R 2< and R 1< are different, and R 2< comprises a carbonyl group.

[0430] In some embodiments, R 2< and R 1< are different, and R 2< comprises 1 or 2 (e.g., 1) nitrogen atoms.

[0431] In some embodiments, R 2< and R 1< are different, and R 2< comprises 1 or 2 (e.g., 1) oxygen atoms.

[0432] In some embodiments, R 2< and R 1< are different, and R 2< comprises a sulfur atom.

[0433] In some embodiments, R 1< and R 2< are the same.

[0434] In some embodiments, R 1< is para or meta to R 2< .

[0435] In some embodiments, R 1< is para or ortho to R 2< .

[0436] In some embodiments, R 1< is ortho or meta to R 2< .In some embodiments, R 1< is para to R 2< .

[0437] In some embodiments, R 1< is meta to R 2< .

[0438] In some embodiments, R 1< is ortho to R 2< .The variables o and p

[0439] In some embodiments, o=2.

[0440] In some embodiments, p=0, 1, 2, or 3.

[0441] In some embodiments, p=0.

[0442] In some embodiments, p=1.

[0443] In some embodiments, p=2.

[0444] In some embodiments, o=2 and p=0.

[0445] In some embodiments, o=2 and p=1.

[0446] In some embodiments, o=2 and p=2.

[0447] In some embodiments, o=2 and p=3.The ring B and substitutions on the ring B

[0448] In some embodiments, B is one of the rings disclosed hereinbelow, substituted as disclosed hereinbelow, wherein in each case the bond that is shown as being broken by the wavy line connects B to the NH(CO)group of Formula AA.

[0449] In some embodiments, B is any one of

[0450] In some embodiments, the substituted ring B is

[0451] In some embodiments, the substituted ring B is

[0452] In some embodiments, the substituted ring B is

[0453] In some embodiments, the substituted ring B is

[0454] In some embodiments, the substituted ring B is

[0455] In some embodiments, the substituted ring B is

[0456] In some embodiments, the substituted ring B is

[0457] In some embodiments, the substituted ring B is

[0458] In some embodiments, the substituted ring B is

[0459] In some embodiments, the substituted ring B is

[0460] In some embodiments, the substituted ring B is

[0461] In some embodiments, the substituted ring B is

[0462] In some embodiments, the substituted ring B is

[0463] In some embodiments, the substituted ring B is

[0464] In some embodiments, the substituted ring B is

[0465] In some embodiments, the substituted ring B is

[0466] In some embodiments, the substituted ring B is

[0467] In some embodiments, the substituted ring B is

[0468] In some embodiments, the substituted ring B is

[0469] In some embodiments, the substituted ring B is

[0470] In some embodiments, the substituted ring B is

[0471] In some embodiments, the substituted ring B is

[0472] In some embodiments, the substituted ring B is

[0473] In some embodiments, the substituted ring B is

[0474] In some embodiments, the substituted ring B is

[0475] In some embodiments, the substituted ring B is

[0476] In some embodiments, the substituted ring B is

[0477] In some embodiments, the substituted ring B is

[0478] In some embodiments, the substituted ring B is

[0479] In some embodiments, the substituted ring B is

[0480] In some embodiments, the substituted ring B is The groups R 6< and R 7<

[0481] R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl and 3- to 10-membered heterocycloalkyl, and a C 2 -C 6 alkenyl, wherein R 6< and R 7< are each optionally substituted with one or more substituents independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC 2 -C 6 alkynyl, C 6 -C 10 aryloxy, and S(O 2 )C 1 -C 6 alkyl; and wherein the C 1 -C 6 alkyl or C 1 -C 6 alkoxy that R 6< or R 7< is substituted with is optionally substituted with one or more hydroxyl, C 6 -C 10 aryl or NR 8< R 9< , or wherein R 6< or R 7< is optionally fused to a five- to -seven-membered carbocyclic ring or heterocyclic ring containing one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0482] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl and 3- to 10-membered heterocycloalkyl, and a C 2 -C 6 alkenyl, wherein R 6< and R 7< are each optionally substituted with one or more substituents independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC 2 -C 6 alkynyl, C 6 -C 10 aryloxy, and S(O 2 )C 1 -C 6 alkyl; and wherein the C 1 -C 6 alkyl or C 1 -C 6 alkoxy that R 6< or R 7< is substituted with is optionally substituted with one or more hydroxyl, C 6 -C 10 aryl or NR 8< R 9< , or wherein R 6< or R 7< is optionally fused to a five- to -seven-membered carbocyclic ring or heterocyclic ring containing one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 6 aliphatic carbocyclic ring or at least one 5-to 6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0483] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0484] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0485] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0486] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl, and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are unsubstituted; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0487] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl are each unsubstituted; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0488] In some embodiments, R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; and R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or R 6< and R 7< , taken together with the atoms connecting them, independently form C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0489] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo, or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0490] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo, or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 6 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0491] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo, or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 5-to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0492] In some embodiments, R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo, or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0493] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 6 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0494] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0495] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 5 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0496] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 6 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0497] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 5-to 6-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0498] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 5-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0499] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 6-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0500] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0501] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 5 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0502] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 6 aliphatic carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0503] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 5-to 6-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0504] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 5-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0505] In some embodiments, at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one 6-membered heterocyclic ring containing 1 heteroatom independently selected from O, N, and S, wherein the heterocyclic ring is optionally independently substituted with one or more C 1 -C 6 alkyl.

[0506] In some embodiments, o=2; p=1, 2, or 3; and R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 8 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NH 2 , NHC 1 -C 6 alkyl, N(C 1 -C 6 alkyl) 2 , CONR 8< R 9< , SF 5 , SC 1 -C 6 alkyl, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl, and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein the 3- to 7-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C 1 -C 6 alkyl, and OC 1 -C 6 alkyl.

[0507] In some embodiments, o=2; p=1; and each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; and R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or R 6< and R 7< , taken together with the atoms connecting them, independently form C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0508] In some embodiments, o=2; p=2 or 3; and each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 7 (e.g., C 4 -C 6 ) carbocyclic ring (e.g., aliphatic carbocyclic ring) or at least one 5-to-7-membered (e.g., 5-to-6-membered) heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0509] In some embodiments, o=2; p=1, 2, or 3; and R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo, or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 8 carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more hydroxy or oxo.

[0510] In some embodiments, o=2; p=1, 2, or 3; and R 6< and R 7< are each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, CN, NO 2 , COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , and 3- to 7-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy or oxo.

[0511] In some embodiments, o=2; p=1, 2, or 3; and one R 6< and one R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0512] In some embodiments, o=2; p=1, 2, or 3; and one R 6< and one R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 carbocyclic ring or a 5-to-6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0513] In some embodiments, o=2; p=1, 2, or 3; and one R 6< and one R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is unsubstituted.

[0514] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein each carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0515] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 6 carbocyclic ring or a 5-to-6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0516] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 5 carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0517] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 carbocyclic ring, wherein the carbocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0518] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, one pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 carbocyclic ring, and the other pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 5 carbocyclic ring, wherein each of C 4 and C 5 carbocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0519] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, one pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 5 carbocyclic ring, and the other pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S (e.g., a 5-membered heteorocyclic ring, e.g., 5-membered heterocyclic ring containing 1 heteroatom), wherein each of carbocyclic and heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0520] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is unsubstituted.Particular embodiments wherein o=2; p=1, 2, or 3:

[0521] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is C 1 -C 6 alkyl optionally substituted with one or more halo.

[0522] In some embodiments, at least one R 6< is C 1 -C 6 alkyl and at least one R 7< is C 1 -C 6 alkyl.

[0523] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is methyl.

[0524] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is isopropyl.

[0525] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is C 1 -C 6 alkyl substituted with one or more halo.

[0526] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is trifluoromethyl.

[0527] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is C 3 -C 7 cycloalkyl.

[0528] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is cyclopropyl.

[0529] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is halo.

[0530] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is halo.

[0531] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is chloro.

[0532] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is fluoro.

[0533] In some embodiments, o=2; p=1; at least one R 6< is isopropyl; and R 7< is chloro.

[0534] In some embodiments, o=2; p=1; at least one R 6< is isopropyl; and R 7< is fluoro.

[0535] In some embodiments, o=2; p=2; at least one R 6< is isopropyl; and at least one R 7< is fluoro.

[0536] In some embodiments, o=2; p=2; at least one R 6< is isopropyl; one R 7< is fluoro; and the other R 7< is cyano.

[0537] In some embodiments, o=2; p=3; at least one R 6< is isopropyl; two R 7< are fluoro; and one R 7< is chloro.

[0538] In some embodiments, o=2; p=1; at least one R 6< is ethyl; and R 7< is fluoro.

[0539] In some embodiments, o=2; p=1; one R 6< is isopropyl; the other R 6< is trifluoromethyl; and R 7< is chloro.

[0540] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is cyano.

[0541] In some embodiments, at least one R 6< is isopropyl and at least one R 7< is cyano.

[0542] In some embodiments, o=2; p=1; at least one R 6< is isopropyl; and R 7< is cyano.

[0543] In some embodiments, at least one R 6< is C 3 -C 7 cycloalkyl, and at least one R 7< is C 3 -C 7 cycloalkyl.

[0544] In some embodiments, at least one R 6< is cyclopropyl, and at least one R 7< is cyclopropyl.

[0545] In some embodiments, at least one R 6< is C 3 -C 7 cycloalkyl, and at least one R 7< is halo.

[0546] In some embodiments, at least one R 6< is cyclopropyl and at least one R 7< is halo.

[0547] In some embodiments, at least one R 6< is cyclopropyl and at least one R 7< is chloro.

[0548] In some embodiments, at least one R 6< is cyclopropyl and at least one R 7< is fluoro.

[0549] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is C 1 -C 6 alkoxy optionally substituted with one or more halo.

[0550] In some embodiments, at least one R 6< is isopropyl, and at least one R 7< is C 1 -C 6 alkoxy.

[0551] In some embodiments, at least one R 6< is isopropyl, and at least one R 7< is methoxy.

[0552] In some embodiments, o=2; p=1; at least one R 6< is isopropyl, and R 7< is methoxy.

[0553] In some embodiments, at least one R 6< is C 1 -C 6 alkyl, and at least one R 7< is C 1 -C 6 alkoxy substituted with one or more halo.

[0554] In some embodiments, at least one R 6< is isopropyl, and at least one R 7< is trifluoromethoxy.

[0555] In some embodiments, at least one R 6< is isopropyl, and at least one R 7< is difluoromethoxy.

[0556] In some embodiments, at least one R 6< is halo, and at least one R 7< is C 1 -C 6 haloalkyl optionally substituted with hydroxy.

[0557] In some embodiments, at least one R 6< is halo, and at least one R 7< is C 1 -C 6 haloalkoxy.

[0558] In some embodiments, at least one R 6< is chloro, and at least one R 7< is trifluoromethoxy.

[0559] In some embodiments, at least one R 6< is C 1 -C 6 alkoxy; and at least one R 7< is halo.

[0560] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is C 1 -C 6 alkyl optionally substituted with one or more halo.

[0561] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is methyl.

[0562] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is C 1 -C 6 alkyl substituted with one or more halo.

[0563] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is trifluoromethyl.

[0564] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is C 3 -C 7 cycloalkyl.

[0565] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is cyclopropyl.

[0566] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is halo.

[0567] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is halo.

[0568] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is chloro.

[0569] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is fluoro.

[0570] In some embodiments, o=2; p=l; R 7< is isopropyl; and at least one R 6< is chloro.

[0571] In some embodiments, o=2; p=1; R 7< is isopropyl; and at least one R 6< is fluoro.

[0572] In some embodiments, o=2; p=2; R 7< is isopropyl; and at least one R 6< is fluoro.

[0573] In some embodiments, o=2; p=2; at least one R 7< is isopropyl; one R 6< is fluoro; and the other R 6< is cyano.

[0574] In some embodiments, o=2; p=1; R 7< is ethyl; and at least one R 6< is fluoro.

[0575] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is cyano.

[0576] In some embodiments, at least one R 7< is isopropyl and at least one R 6< is cyano.

[0577] In some embodiments, o=2; p=1; R 7< is isopropyl; and at least one R 6< is cyano.

[0578] In some embodiments, at least one R 7< is C 3 -C 7 cycloalkyl, and at least one R 6< is C 3 -C 7 cycloalkyl.

[0579] In some embodiments, at least one R 7< is cyclopropyl, and at least one R 6< is cyclopropyl.

[0580] In some embodiments, at least one R 7< is C 3 -C 7 cycloalkyl, and at least one R 6< is halo.

[0581] In some embodiments, at least one R 7< is cyclopropyl and at least one R 6< is halo.

[0582] In some embodiments, at least one R 7< is cyclopropyl and at least one R 6< is chloro.

[0583] In some embodiments, at least one R 7< is cyclopropyl and at least one R 6< is fluoro.

[0584] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is C 1 -C 6 alkoxy optionally substituted with one or more halo.

[0585] In some embodiments, at least one R 7< is isopropyl, and at least one R 6< is C 1 -C 6 alkoxy.

[0586] In some embodiments, at least one R 7< is isopropyl, and at least one R 6< is methoxy.

[0587] In some embodiments, o=2; p=1; R 7< is isopropyl, and at least one R 6< is methoxy.

[0588] In some embodiments, at least one R 7< is C 1 -C 6 alkyl, and at least one R 6< is C 1 -C 6 alkoxy substituted with one or more halo.

[0589] In some embodiments, at least one R 7< is isopropyl, and at least one R 6< is trifluoromethoxy.

[0590] In some embodiments, at least one R 7< is halo, and at least one R 6< is C 1 -C 6 haloalkyl optionally substituted with one or more hydroxy.

[0591] In some embodiments, at least one R 7< is halo, and at least one R 6< is C 1 -C 6 haloalkoxy.

[0592] In some embodiments, at least one R 7< is chloro, and at least one R 6< is trifluoromethoxy.

[0593] In some embodiments, at least one R 7< is C 1 -C 6 alkoxy; and at least one R 6< is halo.

[0594] In some embodiments, R 6< and R 7< are each attached to a carbon of an aryl ring B.

[0595] In some embodiments, R 6< and R 7< are each attached to a carbon of a heteroaryl ring B.

[0596] In some embodiments, R 6< is attached to a carbon and R 7< is attached to a nitrogen of a heteroaryl ring B.

[0597] In some embodiments, R 7< is attached to a carbon and R 6< is attached to a nitrogen of a heteroaryl ring B.

[0598] In some embodiments, one R 6< and one R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 5 carbocyclic ring optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0599] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 5 aliphatic carbocyclic ring.

[0600] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 carbocyclic ring optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0601] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 aliphatic carbocyclic ring.

[0602] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 6 aromatic carbocyclic ring.

[0603] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0604] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0605] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 5-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0606] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0607] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0608] In some embodiments, R 6< and R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a 6-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0609] In some embodiments, one R 6< and one R 7< are on adjacent atoms, and taken together with the atoms connecting them, form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the ring is fused to the B ring at the 2- and 3- positions relative to the bond connecting the B ring to the NH(CO)group.

[0610] In some embodiments, o=2; p=2; and one pair of one R 6< and one R 7< , are on adjacent atoms; and said pair of one R 6< and one R 7< taken together with the atoms connecting them form form a C 4 -C 8 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0611] In some embodiments, o=2; p=2; and one pair of one R 6< and one R 7< , are on adjacent atoms; and said pair of one R 6< and one R 7< taken together with the atoms connecting them form form a C 5 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0612] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 4 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0613] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 4 aliphatic carbocyclic ring and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring.

[0614] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0615] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring.

[0616] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 6 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0617] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 6 aliphatic carbocyclic ring.

[0618] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 6 aromatic carbocyclic ring.

[0619] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0620] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0621] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0622] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 6-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0623] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 6-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0624] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a 6-membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0625] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 4-8 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5- to 8-mebered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0626] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0627] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 carbocyclic ring optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a 6-mebered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, optionally substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0628] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms; one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered aliphatic heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0629] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein one of the two rings is fused to the B ring at the 2- and 3- positions relative to the bond connecting the B ring to the NR 3< (CO) group, and the other of the two rings is fused to the Bring at the 5- and 6- positions relative to the bond connecting the B ring to the NH(CO) group.

[0630] In some embodiments, o=2; p=2 or 3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them independently form a C 4 -C 8 carbocyclic ring or a 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein one of the two rings is fused to the B ring at the 2- and 3- positions relative to the bond connecting the B ring to the NR 3< (CO) group, and the other of the two rings is fused to the Bring at the 4- and 5- positions relative to the bond connecting the B ring to the NH(CO) group.

[0631] In some embodiments, o=2; p=2; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring.

[0632] In some embodiments, o=2; p=2; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 4 aliphatic carbocyclic ring, and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring.

[0633] In some embodiments, o=2; p=2; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 4 aliphatic carbocyclic ring.

[0634] In some embodiments, o=2; p=2; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, one pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring, and the other pair of one R 6< and one R 7< taken together with the atoms connecting them form a 5-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S.

[0635] In some embodiments, o=2; p=3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring; and one R 7< is halo (e.g., Cl or F).

[0636] In some embodiments, o=2; p=3; and two pairs, each of one R 6< and one R 7< , are on adjacent atoms, and each pair of one R 6< and one R 7< taken together with the atoms connecting them form a C 5 aliphatic carbocyclic ring; and one R 7< is CN.

[0637] In some embodiments, one R 7< is pyrazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0638] In some embodiments, one R 7< is 3-pyrazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0639] In some embodiments, one R 7< is 4-pyrazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0640] In some embodiments, one R 7< is 5-pyrazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0641] In some embodiments, one R 7< is thiazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0642] In some embodiments, one R 7< is 4-thiazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0643] In some embodiments, one R 7< is 5-thiazolyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0644] In some embodiments, one R 7< is furyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0645] In some embodiments, one R 7< is 2-furyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0646] In some embodiments, one R 7< is thiophenyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0647] In some embodiments, one R 7< is 2-thiophenyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0648] In some embodiments, one R 7< is phenyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0649] In some embodiments, one R 7< is cycloalkenyl (e.g., cyclopentenyl, e.g., 1-cyclopentenyl) and is para to the bond connecting the B ring to the NR 3< (CO) group of Formula AA.

[0650] In some embodiments, one R 7< is phenyl optionally substituted with one or more C 1 -C 6 alkyl (e.g., methyl or propyl, e.g., 2-propyl) optionally substituted with one or more hydroxyl, NR 8< R 9< (e.g., dimethylamino), or C 6 -C 10 aryl (e.g., phenyl, naphthyl, or methylenedioxyphenyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0651] In some embodiments, one R 7< is phenyl optionally substituted with one or more C 1 -C 6 alkoxy (e.g., methoxy) optionally substituted with one or more hydroxyl, NR 8< R 9< (e.g., dimethylamino), or C 6 -C 10 aryl (e.g., phenyl, naphthyl, or methylenedioxyphenyl and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0652] In some embodiments, one R 7< is phenyl optionally substituted with one or more C 6 -C 10 aryloxy (e.g., phenoxy) and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0653] In some embodiments, one R 7< is phenyl optionally substituted with one or more CN and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0654] In some embodiments, one R 7< is phenyl optionally substituted with one or more halo (e.g., F, Cl) and is para to the bond connecting the B ring to the NH(CO) group of Formula AA and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0655] In some embodiments, one R 7< is phenyl optionally substituted with one or more COOC 1 -C 6 alkyl (e.g., CO 2 t-Bu) and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0656] In some embodiments, one R 7< is phenyl optionally substituted with one or more S(O 2 )C 1 -C 6 alkyl (e.g., S(O 2 )methyl) and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0657] In some embodiments, one R 7< is phenyl optionally substituted with one or more 3- to 7-membered heterocycloalkyl (e.g., morpholinyl) and is para to the bond connecting the B ring to the NH(CO) group of Formula AA.

[0658] In some embodiments, one R 7< is phenyl optionally substituted with one or more CONR 8< R 9< (e.g., unsubstituted amido) and is para to the bond connecting the B ring to the NH(CO) groupof Formula AA.

[0659] In some embodiments, one R 7< is phenyl optionally substituted with one or more C 1 -C 6 alkyl (e.g., methyl or propyl, e.g., 2-propyl) and with one or more halo (e.g., F, Cl) and is para to the bond connecting the B ring to the NH(CO) groupof Formula AA and is para to the bond connecting the B ring to the NH(CO) groupof Formula AA.

[0660] In some embodiments, R 6< and R 7< are each attached to a carbon of an aryl ring B.

[0661] In some embodiments of any of the formulae herein, each of R 1< and R 2< is independently selected from the group consisting of C 1 -C 6 alkyl optionally substituted with one or more hydroxy, halo, oxo, or C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, halo, oxo, C 1 -C 6 alkoxy, or C 1 -C 6 alkyl; wherein the C 1 -C 6 alkoxy or C 1 -C 6 alkyl is further optionally substituted with one to three hydroxy, halo, NR 8< R 9< , or oxo; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, halo, oxo, or C 1 -C 6 alkyl wherein the C 1 -C 6 alkoxy or C 1 -C 6 alkyl is further optionally substituted with one to three hydroxy, halo, or oxo; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; CO-C 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; S(O 2 )NR n< R 12< ; S(O)C 1 -C 6 alkyl; and S(O 2 )C 1 -C 6 alkyl.

[0662] In some embodiments of any of the formulae herein, R 1< is selected from the group consisting of 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; S(O 2 )CH 3; and S(O 2 )NR 11< R 12< .

[0663] In some embodiments, R 2< is selected from the group consisting of fluoro, chloro, cyano, methyl; methoxy; ethoxy; isopropyl; 1-hydroxy-2-methylpropan-2-yl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; COCH 3 ; COPh; 2-methoxy-2-propyl; S(O 2 )CH 3; and S(O 2 )NR 11< R 12< .

[0664] In some embodiments, the substituted ring B is and each R 6< is independently selected from the group consisting of: C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4-to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl.

[0665] In some embodiments, the substituted ring B is and each R 6< is independently selected from the group consisting of: C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, and C 3 -C 7 cycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, or oxo.

[0666] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or R 6< and R 7< , taken together with the atoms connecting them, independently form C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0667] Not forming part of the invention, the substituted ring B is R 6< , wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SFs, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or R 6< and R 7< , taken together with the atoms connecting them, independently form C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0668] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy.

[0669] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SFs, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0670] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SFs, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0671] Not forming part of the invention, the substituted ring B is R 6< , wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SFs, S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0672] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or R 6< and R 7< , taken together with the atoms connecting them, independently form a C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< .

[0673] In some embodiments, the substituted ring B is wherein each R 6< is independently selected from C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CO-C 1 -C 6 alkyl; CONR 8< R 9< , and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, CONR 8< R 9< , 4- to 6-membered heterocycloalkyl, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(4- to 6-membered heterocycloalkyl), NHCOC 1 -C 6 alkyl, NHCOC 6 -C 10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(4- to 6-membered heterocycloalkyl), and NHCOC 2 -C 6 alkynyl; wherein each R 7< is independently selected from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, halo, CN, COC 1 -C 6 alkyl, CO 2 C 1 -C 6 alkyl, CO 2 C 3 -C 6 cycloalkyl, OCOC 1 -C 6 alkyl, OCOC 6 -C 10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C 6 -C 10 aryl, 5- to 10-membered heteroaryl, CONR 8< R 9< , SF 5 , S(O 2 )C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl and 4- to 6-membered heterocycloalkyl, wherein the C 1 -C 6 alkyl is optionally substituted with one to two C 1 -C 6 alkoxy; or at least one pair of R 6< and R 7< on adjacent atoms, taken together with the atoms connecting them, independently form at least one C 4 -C 7 carbocyclic ring or at least one 5-to-7-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, NR 8< R 9< , CH 2 NR 8< R 9< , =NR 10< , COOC 1 -C 6 alkyl, C 6 -C 10 aryl, and CONR 8< R 9< ; The group R 3<

[0674] R 3< is hydrogen.The group R 14<

[0675] In some embodiments, R 14< is hydrogen, C 1 -C 6 alkyl, 5- to 10-membered monocyclic or bicyclic heteroaryl or C 6 -C 10 monocyclic or bicyclic aryl, wherein each C 1 -C 6 alkyl, aryl or heteroaryl is optionally independently substituted with 1 or 2 R 6< .

[0676] In some embodiments, R 14< is hydrogen or C 1 -C 6 alkyl.

[0677] In some embodiments, R 14< is hydrogen, 5- to 10-membered monocyclic or bicyclic heteroaryl or C 6 -C 10 monocyclic or bicyclic aryl, wherein each C 1 -C 6 alkyl, aryl or heteroaryl is optionally independently substituted with 1 or 2 R 6< .

[0678] In some embodiments, R 14< is hydrogen.

[0679] In some embodiments, R 14< is C 1 -C 6 alkyl.

[0680] In some embodiments, R 14< is methyl.

[0681] In some embodiments, R 14< is 5- to 10-membered monocyclic or bicyclic heteroaryl optionally independently substituted with 1 or 2 R 6< .

[0682] In some embodiments, R 14< is C 6 -C 10 monocyclic or bicyclic aryl optionally independently substituted with 1 or 2 R 6< .The moiety S(=O)(NHR 3< )=N-

[0683] In some embodiments, the sulfur in the moiety S(=O)(NHR 3< )=N- has (S) stereochemistry.

[0684] In some embodiments, the sulfur in the moiety S(=O)(NHR 3< )=N- has (R) stereochemistry.The group R 10<

[0685] In some embodiments, R 10< is C 1 -C 6 alkyl.

[0686] In some embodiments, R 10< is methyl.

[0687] In some embodiments, R 10< is ethyl.The groups R 8< and R 9<

[0688] In some embodiments, each of R 8< and R 9< at each occurrence is independently selected from hydrogen, C 1 -C 6 alkyl, (C=NR 13< )NR 11< R 12< , S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , COR 13< , CO 2 R 13< and CONR 11< R 12< ; wherein the C 1 -C 6 alkyl is optionally substituted with one or more hydroxy, halo, C 1 -C 6 alkoxy, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, C 3 -C 7 cycloalkyl or 3- to 7-membered heterocycloalkyl; or R 8< and R 9< taken together with the nitrogen they are attached to form a 3- to 7-membered ring optionally containing one or more heteroatoms in addition to the nitrogen they are attached to.

[0689] In some embodiments, each of R 8< and R 9< at each occurrence is independently selected from hydrogen, C 1 -C 6 alkyl, (C=NR 13< )NR 11< R 12< , S(O 2 )C 1 -C 6 alkyl, S(O 2 )NR 11< R 12< , COR 13< , CO 2 R 13< and CONR 11< R 12< , wherein the C 1 -C 6 alkyl is optionally substituted with one or more hydroxy, halo, C 1 -C 6 alkoxy, C 6 -C 10 aryl, 5- to 10-membered heteroaryl, C 3 -C 7 cycloalkyl or 3- to 7-membered heterocycloalkyl; or R 8< and R 9< taken together with the nitrogen they are attached to form a 3- to 7-membered ring optionally containing one or more heteroatoms in addition to the nitrogen they are attached to.

[0690] In some embodiments, each of R 8< and R 9< at each occurrence is hydrogen,

[0691] In some embodiments, each R 8< at each occurrence is hydrogen and each R 9< at each occurrence is C 1 -C 6 alkyl.

[0692] In some embodiments, each R 8< at each occurrence is hydrogen and each R 9< at each occurrence is methyl.

[0693] In some embodiments, each R 8< at each occurrence is hydrogen and each R 9< at each occurrence is ethyl.

[0694] In some embodiments, each of R 8< and R 9< at each occurrence is methyl.

[0695] In some embodiments, each of R 8< and R 9< at each occurrence is ethyl.

[0696] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 3-membered ring.

[0697] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 4-membered ring.

[0698] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 5-membered ring.

[0699] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 6-membered ring optionally containing one or more oxygen atoms in addition to the nitrogen they are attached to.

[0700] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 6-membered ring optionally containing one or more nitrogen atoms in addition to the nitrogen they are attached to.

[0701] In some embodiments, R 8< and R 9< taken together with the nitrogen they are attached to form a 7-membered ring.The group R 13<

[0702] In some embodiments, R 13< is C 1 -C 6 alkyl.

[0703] In some embodiments, R 13< is methyl.

[0704] In some embodiments, R 13< is ethyl.

[0705] In some embodiments, R 13< is C 6 -C 10 aryl.

[0706] In some embodiments, R 13< is phenyl.

[0707] In some embodiments, R 13< is 5- to 10-membered heteroaryl.The groups R 11< and R 12<

[0708] In some embodiments, each of R 11< and R 12< at each occurrence is independently selected from hydrogen and C 1 -C 6 alkyl.

[0709] In some embodiments, each of R 11< and R 12< at each occurrence is hydrogen,

[0710] In some embodiments, each R 11< at each occurrence is hydrogen and each R 12< at each occurrence is C 1 -C 6 alkyl.

[0711] In some embodiments, each R 11< at each occurrence is hydrogen and each R 12< at each occurrence is methyl.

[0712] In some embodiments, each R 11< at each occurrence is hydrogen and each R 12< at each occurrence is ethyl.

[0713] In some embodiments, each of R 11< and R 12< at each occurrence is methyl.

[0714] In some embodiments, each of R 11< and R 12< at each occurrence is ethyl.

[0715] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0716] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0717] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0718] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0719] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0720] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0721] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0722] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0723] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0724] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0725] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0726] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0727] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0728] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0729] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0730] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0731] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0732] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0733] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0734] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0735] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0736] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0737] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0738] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0739] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0740] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0741] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0742] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0743] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0744] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 . the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0745] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0746] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO-5- to 10-membered heteroaryl; CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0747] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0748] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; 3- to 7-membered heterocycloalkyl substituted with one or more NR 8< R 9< ; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; and S(O 2 )C 1 -C 6 alkyl.

[0749] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 .

[0750] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOCi-C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; and S(O 2 )C 1 -C 6 alkyl. the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; (dimethylamino)methyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; and S(O 2 )CH 3 . the substituted ring A is and R 1< is selected from: C 1 -C 6 alkyl optionally substituted with one or more hydroxy; C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy; C 1 -C 6 alkyl substituted with one or more oxo; C 3 -C 7 cycloalkyl substituted with one or more oxo; C 1 -C 6 alkyl substituted with one or more C 1 -C 6 alkoxy; C 3 -C 7 cycloalkyl substituted with one or more C 1 -C 6 alkoxy; C 1 -C 6 haloalkyl; C 1 -C 6 alkoxy; C 1 -C 6 haloalkoxy; halo; CN; NO 2 ; COC 1 -C 6 alkyl; CO-C 6 -C 10 aryl; CO(5- to 10-membered heteroaryl); CO 2 C 1 -C 6 alkyl; CO 2 C 3 -C 8 cycloalkyl; OCOC 1 -C 6 alkyl; OCOC 6 -C 10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C 6 -C 10 aryl; 5- to 10-membered heteroaryl; NH 2 ; NHC 1 -C 6 alkyl; N(C 1 -C 6 alkyl) 2 ; CONR 8< R 9< ; SF 5 ; C 1 -C 6 alkyl substituted with one or more NR 8< R 9< ; and S(O 2 )C 1 -C 6 alkyl. the substituted ring A is and R 1< is selected from: 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH 3 ; COCH 2 CH 3 ; 2-methoxy-2-propyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; (dimethylamino)methyl; and S(O 2 )CH 3 .

[0751] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo.

[0752] In some embodiments of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0753] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C l o aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C l o aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl. R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo.

[0754] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0755] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C l o aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C l o aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0756] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl; R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0757] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C l o aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C l o aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0758] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0759] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C l o aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0760] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0761] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C l o aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C l o aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0762] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0763] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0764] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0765] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0766] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0767] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0768] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0769] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0770] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0771] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0772] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0773] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is COCH 3 , and R 1< is methyl; or R 2< is 2-methoxy-2-propyl, and R 1< is methyl.

[0774] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0775] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-propyl and R 2< is fluoro; R 1< is 1-hydroxy-1-cyclopropyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclobutyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclopentyl, and R 2< is methyl; R 1< is 1-hydroxy-1-cyclohexyl, and R 2< is methyl; R 1< is morpholinyl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is methyl; R 1< is 1,3-dioxolan-2-yl, and R 2< is fluoro; R 1< is 1,3-dioxolan-2-yl, and R 2< is chloro; R 1< is COCH 3 , and R 2< is methyl; R 1< is 2-methoxy-2-propyl, and R 2< is methyl; R 1< is (dimethylamino)methyl, and R 2< is methyl. R 2< is 1-hydroxy-2-methylpropan-2-yl, and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is isopropyl; R 2< is 2-hydroxy-2-propyl and R 1< is 1-hydroxyethyl; R 2< is hydroxymethyl and R 1< is methyl; R 2< is 1-hydroxyethyl and R 1< is methyl; R 2< is 2-hydroxyethyl and R 1< is methyl; R 2< is 1-hydroxy-2-propyl and R 1< is methyl; R 2< is 2-hydroxy-2-propyl and R 1< is phenyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is 2-hydroxy-2-propyl and R 1< is pyridyl; R 2< is 2-hydroxy-2-propyl and R 1< is pyrazolyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )CH 3 ; R 2< is 2-hydroxy-2-propyl and R 1< is chloro; R 2< is 2-hydroxy-2-propyl and R 1< is fluoro; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 1-hydroxy-1-cyclopropyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclobutyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclopentyl, and R 1< is methyl; R 2< is 1-hydroxy-1-cyclohexyl, and R 1< is methyl; R 2< is morpholinyl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is methyl; R 2< is 1,3-dioxolan-2-yl, and R 1< is fluoro; R 2< is 1,3-dioxolan-2-yl, and R 1< is chloro; R 2< is (dimethylamino)methyl, and R 1< is methyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is COCH 3 , and R 1< is methyl.

[0776] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is C 6 -C 10 aryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is 5- to 10-membered heteroaryl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is SF 5 ; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is S(O 2 )C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is C 1 -C 6 alkyl; R 1< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 2< is halo; R 1< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 2< is methyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is C 1 -C 6 alkyl; R 1< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 2< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is C 6 -C 10 aryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is 5- to 10-membered heteroaryl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is SF 5 . R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is S(O 2 )C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 3 -C 7 cycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is C 1 -C 6 alkyl; R 2< is 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is C 1 -C 6 alkyl; R 2< is C 1 -C 6 alkyl optionally substituted with one or more NR 8< R 9< , and R 1< is halo; R 2< is C 1 -C 6 alkyl optionally substituted with one or more oxo, and R 1< is methyl; or R 2< is C 1 -C 6 alkyl optionally substituted with one or more C 1 -C 6 alkoxy, and R 1< is C 1 -C 6 alkyl.

[0777] In some embodiments, of the compound of formula AA, the substituted ring A is and R 1< and R 2< are one of the following combinations: R 1< is 1-hydroxy-2-methylpropan-2-yl, and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is isopropyl; R 1< is 2-hydroxy-2-propyl and R 2< is 2-hydroxy-2-propyl; R 1< is 2-hydroxy-2-propyl and R 2< is 1-hydroxyethyl; R 1< is hydroxymethyl and R 2< is methyl; R 1< is 1-hydroxyethyl and R 2< is methyl; R 1< is 2-hydroxyethyl and R 2< is methyl; R 1< is 1-hydroxy-2-propyl and R 2< is methyl; R 1< is 2-hydroxy-2-propyl and R 2< is phenyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyridyl; R 1< is 2-hydroxy-2-propyl and R 2< is pyrazolyl; R 1< is 2-hydroxy-2-propyl, and R 2< is S(O 2 )CH 3 ; R 1< is 2-hydroxy-2-propyl and R 2< is chloro; R 1< is 2-hydroxy-2-pr...

Claims

1. A compound of Formula AA wherein m = 0, 1, or 2; n = 0, 1, or 2; o = 2; p = 0, 1, 2, or 3, wherein A is a 5- to 10-membered monocyclic or bicyclic heteroaryl or a C6-C10 monocyclic or bicyclic aryl; B is any one of wherein R1 and R2 are each independently selected from C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, Ci-C6 haloalkoxy, halo, CN, NO2, COC1-C6 alkyl, CO-C6-C10 aryl; CO(5- to 10-membered heteroaryl); CO2C1-C6 alkyl, CO2C3-C8 cycloalkyl, OCOC1-C6 alkyl, OCOC6-C10 aryl, OCO(5-to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C6-C10 aryl, 5- to 10-membered heteroaryl, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, NHCOC1-C6 alkyl, NHCOC6-C10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC2-C6 alkynyl, NHCOOCC1-C6 alkyl, NH-(C=NR13)NR11R12, CONR8R9, SF5, SC1-C6 alkyl, S(O2)C1-C6 alkyl, S(O)C1-C6 alkyl, S(O2)NR11R12, C3-C7 cycloalkyl and 3- to 7-membered heterocycloalkyl, wherein the C1-C6 alkyl, C1-C6 haloalkyl, C3-C7 cycloalkyl and 3- to 7-membered heterocycloalkyl is optionally substituted with one or more substituents each independently selected from hydroxy, halo, CN, oxo, C1-C6 alkyl, C1-C6 alkoxy, NR8R9, =NR10, COOC1-C6 alkyl, CONR8R9, 3- to 7-membered heterocycloalkyl, C6-C10 aryl, 5- to 10-membered heteroaryl, OCOC1-C6 alkyl, OCOC6-C10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC1-C6 alkyl, NHCOC6-C10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), and NHCOC2-C6 alkynyl; wherein each C1-C6 alkyl substituent and each C1-C6 alkoxy substituent of the R1 or R2 C3-C7 cycloalkyl or of the R1 or R2 3- to 7-membered heterocycloalkyl is further optionally independently substituted with one to three hydroxy, halo, NR8R9, or oxo; wherein the 3- to 7-membered heterocycloalkyl, C6-C10 aryl, 5- to 10-membered heteroaryl, NHCOC6-C10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C1-C6 alkyl, and OC1-C6 alkyl; or at least one pair of R1 and R2 on adjacent atoms, taken together with the atoms connecting them, independently form at least one C4-C8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, halo, oxo, C1-C6 alkyl, C1-C6 alkoxy, NR8R9, =NR10, COOC1-C6 alkyl, C6-C10 aryl, and CONR8R9 wherein the C1-C6 alkyl and C1-C6 alkoxy are optionally substituted with hydroxy, halo, oxo, NR8R9, =NR10, COOC1-C6 alkyl, C6-C10 aryl, and CONR8R9; R6 and R7 are each independently selected from C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, Ci-C6 haloalkoxy, halo, CN, NO2, COC1-C6 alkyl, CO2C1-C6 alkyl, CO2C3-C8 cycloalkyl, OCOCi-C6 alkyl, OCOC6-C10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), C6-C10 aryl, 5- to 10-membered heteroaryl, NH2, NHC1-C6 alkyl, N(C1-C6 alkyl)2, CONR8R9, SF5, S(O2)C1-C6 alkyl, C3-C10 cycloalkyl and 3- to 10-membered heterocycloalkyl, and a C2-C6 alkenyl, wherein R6 and R7 are each optionally substituted with one or more substituents independently selected from hydroxy, halo, CN, oxo, C1-C6 alkyl, C1-C6 alkoxy, NR8R9, =NR10, COOC1-C6 alkyl, CONR8R9, 3- to 7-membered heterocycloalkyl, C6-C10 aryl, 5- to 10-membered heteroaryl, OCOC1-C6 alkyl, OCOC6-C10 aryl, OCO(5- to 10-membered heteroaryl), OCO(3- to 7-membered heterocycloalkyl), NHCOC1-C6 alkyl, NHCOC6-C10 aryl, NHCO(5- to 10-membered heteroaryl), NHCO(3- to 7-membered heterocycloalkyl), NHCOC2-C6 alkynyl, C6-C10 aryloxy, and S(O2)C1-C6 alkyl; and wherein the C1-C6 alkyl or C1-C6 alkoxy that R6 or R7 is substituted with is optionally substituted with one or more hydroxyl, C6-C10 aryl or NR8R9, or wherein R6 or R7 is optionally fused to a five- to -seven-membered carbocyclic ring or heterocyclic ring containing one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; wherein the 3- to 7-membered heterocycloalkyl, C6-C10 aryl, 5- to 10-membered heteroaryl, NHCOC6-C10 aryl, NHCO(5- to 10-membered heteroaryl) and NHCO(3- to 7-membered heterocycloalkyl) are optionally substituted with one or more substituents independently selected from halo, C1-C6 alkyl, and OC1-C6 alkyl; or at least one pair of R6 and R7 on adjacent atoms, taken together with the atoms connecting them, independently form at least one C4-C8 carbocyclic ring or at least one 5- to 8-membered heterocyclic ring containing 1 or 2 heteroatoms independently selected from O, N, and S, wherein the carbocyclic ring or heterocyclic ring is optionally independently substituted with one or more substituents independently selected from hydroxy, hydroxymethyl, halo, oxo, C1-C6 alkyl, C1-C6 alkoxy, NR8R9, CH2NR8R9, =NR10, COOC1-C6 alkyl, C6-C10 aryl, and CONR8R9; each of R4 and R5 is independently selected from hydrogen and C1-C6 alkyl; R10 is C1-C6 alkyl; each of R8 and R9 at each occurrence is independently selected from hydrogen, C1-C6 alkyl, (C=NR13)NR11R12, S(O2)C1-C6 alkyl, S(O2)NR11R12, COR13, CO2R13 and CONR11R12, wherein the C1-C6 alkyl is optionally substituted with one or more hydroxy, halo, C1-C6 alkoxy, C6-C10 aryl, 5- to 10-membered heteroaryl, C3-C7 cycloalkyl or 3- to 7-membered heterocycloalkyl; or R8 and R9 taken together with the nitrogen they are attached to form a 3- to 7-membered ring optionally containing one or more heteroatoms in addition to the nitrogen they are attached to; R13 is C1-C6 alkyl, C6-C10 aryl, or 5- to 10-membered heteroaryl; each of R11 and R12 at each occurrence is independently selected from hydrogen and C1-C6 alkyl; R3 is hydrogen; and R14 is hydrogen, C1-C6 alkyl, 5- to 10-membered monocyclic or bicyclic heteroaryl or C6-C10 monocyclic or bicyclic aryl, wherein each C1-C6 alkyl, aryl or heteroaryl is optionally independently substituted with 1 or 2 R6, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1, wherein A is a 5- to 6-membered monocyclic heteroaryl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2; optionally wherein A is any one of: furanyl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2; thiophenyl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2; oxazolyl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2; thiazolyl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2; phenyl optionally substituted with 1 or 2 R1 and optionally substituted with 1 or 2 R2.

3. The compound of claim 1 or 2, wherein m=1 and n=0; optionally wherein A is any one of: or 4. The compound of any one of claims 1 to 3, wherein m=1 and n=1; optionally wherein A is any one of:

5. The compound of any one of claims 1 to 3, wherein m=2 and n=1; optionally wherein A is any one of:

6. The compound of any one of claims 1 to 5, wherein each of R1 and R2, when present, is independently selected from the group consisting of C1-C6 alkyl optionally substituted with one or more hydroxy, halo, oxo, C1-C6 alkoxy, or NR8R9; C3-C7 cycloalkyl optionally substituted with one or more hydroxy, halo, oxo, C1-C6 alkoxy, C1-C6 alkyl, or NR8R9 wherein the C1-C6 salkoxy or C1-C6 alkyl is further optionally substituted with one to three hydroxy, halo, NR8R9, or oxo; 3- to 7-membered heterocycloalkyl optionally substituted with one or more hydroxy, halo, oxo, C1-C6 alkyl, or NR8R9 wherein the Ci-C6 alkoxy or C1-C6 alkyl is further optionally substituted with one to three hydroxy, halo, NR8R9, or oxo; C1-C6 haloalkyl; C1-C6 alkoxy; C1-C6 haloalkoxy; halo; CN; CO-C1-C6 alkyl; CO-C6-C10 aryl; CO(5- to 10-membered heteroaryl); CO2C1-C6 alkyl; CO2C3-C8 cycloalkyl; OCOC1-C6 alkyl; OCOC6-C10 aryl; OCO(5- to 10-membered heteroaryl); OCO(3- to 7-membered heterocycloalkyl); C6-C10 aryl; 5- to 10-membered heteroaryl; NH2; NHC1-C6 alkyl; N(C1-C6 alkyl)2; CONR8R9; SF5; S(Oa)NR11R12, S(O)C1-C6 alkyl; and S(O2)C1-C6 alkyl.

7. The compound of any one of claims 1 to 5, wherein R1 is selected from the group consisting of 1-hydroxy-2-methylpropan-2-yl; methyl; isopropyl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; 1-hydroxy-1-cyclobutyl; 1-hydroxy-1-cyclopentyl; 1-hydroxy-1-cyclohexyl; morpholinyl; 1,3-dioxolan-2-yl; COCH3; COCH2CH3; 2-methoxy-2-propyl; (dimethylamino)methyl; 1-(dimethylamino)ethyl; fluoro; chloro; phenyl; pyridyl; pyrazolyl; S(O2)CH3; and S(O2)NR11R12.

8. The compound of claim 6 or 7, wherein R2 is selected from the group consisting of fluoro, chloro, cyano, methyl; methoxy; ethoxy; isopropyl; 1-hydroxy-2-methylpropan-2-yl; 2-hydroxy-2-propyl; hydroxymethyl; 1-hydroxyethyl; 2-hydroxyethyl; 1-hydroxy-2-propyl; 1-hydroxy-1-cyclopropyl; COCH3; COPh; 2-methoxy-2-propyl; (dimethylamino)methyl; S(O2)CH3; and S(O2)NR11R12.

9. The compound of any one of the preceding claims, wherein B is phenyl substituted with 2 R6 and optionally substituted with 1, 2, or 3 R7.

10. A compound according to claim 1 selected from the group consisting of the compounds below: CompoundStructure101' 101 102 103' 103 104 105 106 107 108 109 110 111 112 113 114 115 117 118 119 120 121 122 123 124 125 126 127 128 129 130 131 132 133 134 135 136 137 138 139 143 144 145 146 147 148 149 150 151 152 153 154 155 156 157 158 159 160 161 163 164 165 166 167 168 169 170 171 172 172a 172b 173 173a 173b 174 175 176 176a 176b 177 177a 177b 178 178a 178b 179 179a 179b 180 180a 180b 181 181a 181b 182 182a 182b 183 183a 183b 184 185 185a 185b 186 186a 186b 187 187a 187b 188 188a 188b 189 189a 189b 190 190a 190b 191 192 192a 192b 193 193a 193b CompoundStructure105a 105b 106a 106b 107a 107b 108a 108b 109a 109b 110a 110b 112a 112b 120a 120b 121a 121b 122a 122b 125a 125b 129a 129b 130a 130b 131a 131b 134a 134b 135a 135b 136a 136b 143a 143b 144a 144b 145a 145b 148a 148b 149a 149b 151a' 151b' 151a 151b 152a 152b 153a 153b 154a 154b 157a 157b 158a 158b 161a 161b 165a 165b 167a 167b 168a 168b 170a 170b 171a 171b 174a 174b 191a 191b 195 195a 195ba 195bb 196 197 198 200 202 202a 202b 205 205a 205b 206 206a 206b 207 207a 207b 208 209 211 212 212a 212b 213 216 220 220a 220b 221 223a 223b 225a 225b 113a 113b 137a 137b 138a 138b 139a 139b 159a 159ba 159ab 195e 207bb 207aa 207c 303 303a 303b 306 307 308 308a 308b 309 310 311 312 313 314 315 315b 315a 316 316b 317 317ab 317aa 317bb 317ba 318 318a 318b 319 319ab 319ba 319aa 319bb 320 320a 320b 321 321b 321a 322 323 323ab 323aa 323bb 323ba 325 325a 325b 326 326b 326a 327 328b 328a 329 329a 329b 330 330a 330b 332 332a 332b 333 333a 333b 334 334ba 334bb 334aa 334ab 334b 334a 335 335b 335a 336 336a 336b 337 337b 338 338a 339a 340 340a 340b 341 341b 342 343 343a 343b 344 345 346 347 348 349 350 351 352 352b 352a 354 354a 354b 355 356 357 357a 357b 358 359 359a 360ba 360bb 363b 363a 364a 364b 365a 365b 366a 366b 367a 367b 369a 369b 371b 372b 373b 375 375a 375b 376 376a 376b 377 378 379 379a 379b 380 380a 380b 380c 380d 382 382a 382b 383 383a 383b 384a 384b 387a 387b or a pharmaceutically acceptable salt thereof.

11. The compound according to claim 1 selected from the group consisting of 101' 101 102 or a pharmaceutically acceptable salt thereof.

12. The compound according to claim 1 selected from the group consisting of 103' 103 104 or a pharmaceutically acceptable salt thereof.

13. The compound according to claim 1 selected from the group consisting of 108 or a pharmaceutically acceptable salt thereof.

14. The compound according to claim 1 selected from the group consisting of 186 186a 186b or a pharmaceutically acceptable salt thereof.

15. The compound according to claim 1 selected from the group consisting of 326 or a pharmaceutically acceptable salt thereof.

16. The compound according to claim 1 selected from the group consisting of 187 187a 187b or a pharmaceutically acceptable salt thereof.

17. The compound of any one of the preceding claims, wherein the sulfur in the moiety S(=O)(NHR3)=N- has (S) stereochemistry.

18. The compound of any one of claims 1 to 16, wherein the sulfur in the moiety S(=O)(NHR3)=N- has (R) stereochemistry.

19. A pharmaceutical composition comprising a compound or salt as claimed in any one of claims 1 to 18 and one or more pharmaceutically acceptable excipients.

20. The compound of any one of claims 1 to 18 for use in the treatment of a disease, disorder or condition that is any one of: a metabolic disorder, optionally wherein the metabolic disorder is Type 2 diabetes, atherosclerosis, obesity or gout; a disease of the central nervous system, optionally wherein the disease of the central nervous system is Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease; lung disease, optionally wherein the lung disease is asthma, COPD or pulmonary idiopathic fibrosis; liver disease, optionally wherein the liver disease is NASH syndrome, viral hepatitis or cirrhosis; pancreatic disease, optionally wherein the pancreatic disease is acute pancreatitis or chronic pancreatitis; kidney disease, optionally wherein the kidney disease is acute kidney injury or chronic kidney injury; intestinal disease, optionally wherein the intestinal disease is Crohn's disease or Ulcerative Colitis; skin disease, optionally wherein the skin disease is psoriasis; musculoskeletal disease, optionally wherein the musculoskeletal disease is scleroderma; a vessel disorder, optionally wherein the vessel disorder is giant cell arteritis; a disorder of the bones, optionally wherein the disorder of the bones is osteoarthritis, osteoporosis or osteopetrosis disorders; eye disease, optionally wherein the eye disease is glaucoma or macular degeneration a disease caused by viral infection, optionally wherein the diseases caused by viral infection is HIV or AIDS; an autoimmune disease, optionally wherein the autoimmune disease is Rheumatoid Arthritis, Systemic Lupus Erythematosus, Autoimmune Thyroiditis cancer or aging, optionally wherein the disorder or condition that is cancer is selected from: myelodysplastic syndromes (MDS); non-small cell lung cancer, such as non-small cell lung cancer in patients carrying mutation or overexpression of NLRP3; acute lymphoblastic leukemia (ALL), such as ALL in patients resistant to glucocorticoids treatment; Langerhan's cell histiocytosis (LCH); multiple myeloma; promyelocytic leukemia; acute myeloid leukemia (AML); chronic myeloid leukemia (CML); gastric cancer; and lung cancer metastasis.

21. The compound for use according to claim 20, further comprising administering a therapeutically effective amount of an anti-TNFα agent to the subject; optionally wherein: the NLRP3 antagonist is administered to the subject prior to administration of the anti-TNFα agent to the subject; or wherein the anti-TNFα agent is administered to the subject prior to the administration of the NLRP3 antagonist to the subject; or wherein the NLRP3 antagonist and the anti-TNFα agent are administered to the subject at substantially the same time.